HECTOROL
Clinical safety rating: caution
Comprehensive clinical and safety monograph for HECTOROL (HECTOROL).
Synthetic vitamin D analog that binds to vitamin D receptors (VDR), increasing intestinal absorption of calcium and phosphate, and promoting bone mineralization. Also suppresses parathyroid hormone (PTH) production.
| Metabolism | Hepatic via CYP27A1 and CYP3A4; undergoes further metabolism to active and inactive metabolites. |
| Excretion | Primarily hepatic metabolism followed by biliary excretion; renal excretion accounts for <2% of unchanged drug. |
| Half-life | Terminal elimination half-life is approximately 5.0 hours in healthy adults; prolonged in patients with hepatic impairment. |
| Protein binding | ≥99.9% bound to plasma proteins, primarily vitamin D-binding protein (DBP). |
| Volume of Distribution | 1.4 L/kg; indicates extensive distribution into tissues, including bone and parathyroid glands. |
| Bioavailability | Oral: approximately 70%; limited data available for other routes. |
| Onset of Action | Oral: 2-6 hours for elevation of serum calcium; intravenous: within 12 hours for suppression of PTH. |
| Duration of Action | Oral: 1-2 days for maximal effect on serum calcium; intravenous: up to 4 days for PTH suppression. |
0.5 to 1.5 mcg intravenously three times weekly during hemodialysis; adjust to maintain serum intact PTH within target range (1.5 to 3 times upper limit of normal). Initial dose: 0.5 mcg three times weekly; may increase by 0.25 to 0.5 mcg at 2- to 4-week intervals.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for GFR-based impairment; HECTOROL is indicated for patients on chronic hemodialysis. In predialysis CKD, use is not recommended. No specific GFR-based adjustments provided. |
| Liver impairment | No specific dose adjustments for hepatic impairment based on Child-Pugh classification have been established. Use with caution in severe hepatic impairment due to potential altered vitamin D metabolism. |
| Pediatric use | Safety and effectiveness in pediatric patients have not been established; no recommended pediatric dosing available. |
| Geriatric use | No specific dose adjustments for geriatric patients; clinical studies did not include sufficient numbers of subjects aged 65 and over to determine differences in response. Use with monitoring of serum calcium, phosphorus, and intact PTH. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for HECTOROL (HECTOROL).
| Breastfeeding | Excretion in human milk unknown; M/P ratio not available. Avoid use during breastfeeding unless maternal need clearly outweighs risk; consider alternative vitamin D analogs if possible. |
| Teratogenic Risk | Category C. First trimester: Potential risk of hypercalcemia-related fetal harm; limited human data. Second/third trimesters: Risk of fetal hypercalcemia, suppression of fetal parathyroid function, and possible craniofacial malformations at high doses. |
| Fetal Monitoring |
■ FDA Black Box Warning
None.
| Serious Effects |
["Hypercalcemia","Vitamin D toxicity","Hypersensitivity to doxercalciferol or any of its components"]
| Precautions | ["Hypercalcemia and hyperphosphatemia risk; monitor serum calcium and phosphorus levels.","Adynamic bone disease with oversuppression of PTH.","Digitalis toxicity potentiated by hypercalcemia.","Aluminum hydroxide and magnesium-containing antacids may bind to the drug."] |
Loading safety data…
| Monitor maternal serum calcium, phosphorus, and alkaline phosphatase every 1-2 weeks; fetal ultrasound for signs of hypercalcemia (e.g., nephrocalcinosis, growth restriction); adjust dose to maintain normocalcemia. |
| Fertility Effects | No known direct adverse effects on fertility in animal studies; clinical data insufficient to assess impact on human fertility. |